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Medchemcomm. 2017 Sep 14;8(11):2060-2066. doi: 10.1039/c7md00354d. eCollection 2017 Nov 1.

Synergism of fused bicyclic 2-aminothiazolyl compounds with polymyxin B against Klebsiella pneumoniae.

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Shanghai Key Laboratory of Chemical Biology , School of Pharmacy , East China University of Science and Technology , Shanghai 200237 , China . Email: ; ; Tel: +86 21 64252945.
School of Pharmacy , Shanghai Jiaotong University , China.
Shanghai Institute of Pharmaceutical Industry , China.
Shanghai Collaborative Innovation Center for Biomanufacturing Technology , Shanghai 200237 , China.


A series of fused bicyclic 2-aminothiazolyl compounds were synthesized and evaluated for their synergistic effects with polymyxin B (PB) against Klebsiella pneumoniae (SIPI-KPN-1712). Some of the synthesized compounds exhibited synergistic activity. When 4 μg ml-1 compound B1 was combined with PB, it showed potent antibacterial activity, achieving 64-fold reduction of the MIC of PB. Furthermore, compound B1 showed prominent synergistic efficacy in both concentration gradient and time-kill curves in vitro. In addition, B1 combined with PB also exhibited synergistic and partial synergistic effect against E. coli (ATCC25922 and its clinical isolates), Acinetobacter baumannii (ATCC19606 and its clinical isolates), and Pseudomonas aeruginosa (Pae-1399).

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